The inhibition of essential enzymes in microbial pathogens offers a route to treatment of infectious diseases. However, although the biology of the organism dictates a need for a particular enzyme activity, this does not necessarily mean that the enzyme is a good drug target. The chemistry of the active site (size, shape and properties) determines the likelihood of finding a molecule with the right properties to influence drug discovery. Discriminating between good and less-good targets is important. Studies on enzymes involved in the regulation of oxidative stress and pterin/folate metabolism of trypanosomatid parasites and isoprenoid precursor biosynthesis in bacteria and apicomplexan parasites illustrates a range of active sites representing those that are challenging with respect to the discovery of potent inhibitors, to others that provide more promising opportunities in drug discovery.
Conference Article| October 25 2007
Picking pockets to fuel antimicrobial drug discovery
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W.N. Hunter; Picking pockets to fuel antimicrobial drug discovery. Biochem Soc Trans 1 November 2007; 35 (5): 980–984. doi: https://doi.org/10.1042/BST0350980
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